Title:
PHOSPHORAMIDITE ACTIVATOR
Document Type and Number:
WIPO Patent Application WO/2021/075423
Kind Code:
A1
Abstract:
The present invention addresses the problem of providing a phosphoramidite activator which improves the solubility of 5-benzylthio-1H-tetrazole in acetonitrile without lowering the yield and purity of a target product. The present invention relates to: a phosphoramidite activator which contains (i) at least one compound that is selected from the group consisting of piperidine, pyrrolidine, N-alkyl piperidine and N-alkyl pyrrolidine, (ii) 5-benzylthio-1H-tetrazole and (iii) acetonitrile; and a method for activating phosphoramidite and a method for synthesizing a phosphoric acid ester or a thiophosphoric acid ester, said methods using the above-described activator.
Inventors:
KIKUCHI SEIHO (JP)
SANO KIMIHIKO (JP)
SANO KIMIHIKO (JP)
Application Number:
PCT/JP2020/038612
Publication Date:
April 22, 2021
Filing Date:
October 13, 2020
Export Citation:
Assignee:
FUJIFILM WAKO PURE CHEMICAL CORP (JP)
International Classes:
C07H1/02; C07H23/00
Foreign References:
| JP2008530092A | 2008-08-07 | |||
| JP2007531794A | 2007-11-08 | |||
| JP2008530092A | 2008-08-07 |
Other References:
BRILL; K-D; ET AL: "Synthesis of Deoxydinucleoside Phosphorodithioates", AMERICAN CHEMICAL SOCIETY, vol. 113, no. 10, 1991, pages 3972 - 3980, XP002275212, DOI: 10.1021/ja00010a045
SANGHVI; Y S; ET AL: "Improved process for the preparation of nucleosidic phosphoramidites using asafer and cheaper activator", ORG. PROC. RES. DEV., vol. 4, no. 3, 2000, pages 175 - 181, XP002350648, DOI: 10.1021/op990086k
J. AM. CHEM. SOC., vol. 132, 2010, pages 15930
See also references of EP 4047004A4
SANGHVI; Y S; ET AL: "Improved process for the preparation of nucleosidic phosphoramidites using asafer and cheaper activator", ORG. PROC. RES. DEV., vol. 4, no. 3, 2000, pages 175 - 181, XP002350648, DOI: 10.1021/op990086k
J. AM. CHEM. SOC., vol. 132, 2010, pages 15930
See also references of EP 4047004A4
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